Inflammation/Immunology

PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a K_d of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity.

Vismodegib (GDC-0449) is a BBB-permeable and orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC₅₀ values of 3.0 μM and 1.4 μM, respectively.

(R)-GNE-140 is a potent inhibitor of lactate dehydrogenase (LDH) A, B and C, with IC₅₀ values of 3, 5 and 5 nM against LDHA, LDHB, LDHC, respectively. (R)-GNE-140 blocks the conversion of pyruvate to lactate, reduces lactate production and histone lysine lactylation, and inhibits glycolysis. (R)-GNE-140 attenuates cardiac hypertrophy, alleviates PM_2.5-induced pulmonary inflammation and fibrosis, blocks MRSA-induced Arg1 expression. (R)-GNE-140 is applicable to research related to pathological cardiac hypertrophy, pulmonary fibrosis, MRSA infection and pancreatic cancer.

Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC₅₀ of 0.1 μM and 1.8 μM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis. Tamoxifen Citrate can also be used to induce gene knockout in CreER transgenic mice.

ATPγS (tetralithium salt) is a P2Y11 receptor agonist, an antioxidant and a neuroprotective agent. ATPγS (tetralithium salt) can be used as a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A. ATPγS (tetralithium salt) is active in ATP hydrolysis.

SB290157 trifluoroacetate is a potent and selective C3a receptor antagonist with an IC₅₀ of 200 nM.

Gallic acid (3,4,5-Trihydroxybenzoic acid) is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2). Gallic acid has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities.

Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID₅₀ of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.

Tezepelumab (anti-TSLP) is human monoclonal antibody (IgG2λ) that binds specifically to TSLP, blocking it from interacting with its heterodimeric receptor. Tezepelumab can be used for the research of severe, uncontrolled asthma.

Trypsin is a serine protease enzyme, and hydrolyzes proteins at the carboxyl side of the Lysine or Arginine. Trypsin activates PAR2 and PAR4. Trypsin induces cell-to-cell membrane fusion in PDCoV infection by the interaction of S glycoprotein of PDCoV and pAPN. Trypsin also promotes cell proliferation and differentiation. Trypsin can be used in the research of wound healing and neurogenic inflammation.

ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC₅₀ of 7 μM.

Angiotensin II human (Angiotensin II) acetate is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human acetate plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis. Angiotensin II human acetate induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway.

BzATP triethylammonium salt acts as a P2X receptor agonist with pEC₅₀s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively. BzATP triethylammonium salt is potent at P2X7 receptors with EC₅₀s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively.

TNF-α (31-45), human is a potent NF-kB pathway activator. TNF-αis a proinflammatory cytokine that induces necrosis or apoptosis. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis.

diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively.

Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC₅₀ of 200 pM. Ceritinib also inhibits IGF-1R, InsR, and STK22D with IC₅₀ values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency.

α-CGRP (mouse, rat), a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP (mouse, rat) can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP (mouse, rat) has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies.

Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent voltage-dependent calcium channel (VDCC) blocker. Ebselen potently inhibits M^pro (IC₅₀=0.67 μM) and COVID-19 virus (EC₅₀=4.67 μM).Ebselen is an inhibitor of HIV-1 capsid CTD dimerization. Ebselen, an organoselenium compound, can permeate the blood-brain barrier and has anti-inflammatory, antioxidant and anticancer activity.

Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM.

5-Aminolevulinic acid (5-ALA; δ-Aminolevulinic acid; 5-Amino-4-oxopentanoic acid) hydrochloride is an orally active heme precursor. 5-Aminolevulinic acid hydrochloride promotes aerobic energy metabolism and increases ATP levels by enhancing the activity of cytochrome c oxidase. 5-Aminolevulinic acid hydrochloride enhances LPS-induced proinflammatory cytokine production and gene activation, and restores the phagocytic activity and ROS generation capacity of neutrophils. 5-Aminolevulinic acid hydrochloride selectively accumulates protoporphyrin IX in tumor cells; as a photosensitizer and radiosensitizer, it induces ROS burst upon light or X-ray irradiation to inhibit tumor growth. 5-Aminolevulinic acid hydrochloride can be applied to the research of septic shock, melanoma, and cancer radiotherapy.